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Application of Periploca forrestii C21 steroides in preparation of IDO (indoleamine-2,3-dioxygenase) inhibitors

A black bone vine, inhibitor technology, used in anti-inflammatory agents, bone diseases, non-central pain relievers, etc.

Active Publication Date: 2018-11-13
NANJING BAOHE BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] For this reason, the technical problem to be solved in the present invention is the problem that there is no C21 steroid in the prior art for the preparation of IDO inhibitors, thereby providing the use of C21 steroids in the preparation of IDO inhibitors

Method used

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  • Application of Periploca forrestii C21 steroides in preparation of IDO (indoleamine-2,3-dioxygenase) inhibitors
  • Application of Periploca forrestii C21 steroides in preparation of IDO (indoleamine-2,3-dioxygenase) inhibitors
  • Application of Periploca forrestii C21 steroides in preparation of IDO (indoleamine-2,3-dioxygenase) inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1 Preparation of C21 steroids of Heigu Teng

[0033] Take the root of Helicobacter sp., pulverize, add 3 times the weight of 95% ethanol aqueous solution and extract at room temperature for 2 times, each extraction for 7 days, combine the extracts, and concentrate under reduced pressure until there is no alcohol smell to obtain Heliconia sp. extract;

[0034] Suspending the Heiguteng extract in 1 times the weight of water, then using chloroform as an extractant to extract twice, collecting the organic phase of the extract, and then concentrating under reduced pressure to obtain the extract of the extract of the Heiguteng chloroform extraction part;

[0035] The extract of the extract from the chloroform extracted part of Heliconia sinensis was purified by silica gel column chromatography. Using petroleum ether as mobile phase A and acetone as mobile phase B, gradient elution was carried out according to the following procedure: first, the volume ratio of A:B wa...

experiment example 1

[0038] Experimental example 1 Study on the inhibitory activity of C21 steroids of the present invention on IDO

[0039] 1. The purpose of the experiment

[0040] HEK293 cells were transfected with plasmid pcDNA3.1-IDO to make it highly express IDO, and then the inhibitory activity of C21 steroids of the present invention on IDO at the cellular level was determined.

[0041] 2. Experimental method

[0042] HEK 293 cells were seeded in a 96-well plate at a density of 2.5×104 cells / well, cultured in DMEM medium (containing 10% fetal bovine serum, 50U / mL penicillin and 50mg / mL streptomycin), placed at 37°C, humidity 95%, 5% CO 2 cultured in an incubator. After culturing for 24 hours, liposome Lipofectamin 2000 was used to mediate pcDNA3.1-hIDO plasmid transfection, and they were divided into positive control group and experimental group 1-2.

[0043] The positive control group used 1-methyltryptophan (1-MT) as the test product, and the experimental groups 1-2 were respective...

experiment example 2

[0053] Experimental example 2 The therapeutic effect of Heigu Teng C21 steroid on ankylosing spondylitis of the present invention

[0054] 1. The purpose of the experiment

[0055] The mouse model of ankylosing spondylitis was established by proteoglycan immunization, and then the C21 steroid of the present invention was administered orally, and the inflammatory markers serum TNF-α and NF-κB receptor activating factor ligand (RANKL) were detected by ELISA. ) level, and the serum IDO activity (Kyn / Trp) was detected to verify the curative effect of the black bone vine C21 steroid on ankylosing spondylitis.

[0056] 2. Experimental method

[0057] 2.1 Experimental animals

[0058] Thirty-two healthy male BALB / c mice, weighing (18±2) g, aged 4-5 weeks, were purchased from Shanghai Slack.

[0059] 2.2 Test drugs

[0060] The salicylic glycoside G and salicylic glycoside I prepared in Example 1 were used as the test drugs.

[0061] 2.3 Experiment grouping and modeling

[006...

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Abstract

The invention belongs to the field of medicines or health products and particularly relates to Periploca forrestii C21 steroides in preparation of IDO (indoleamine-2,3-dioxygenase) inhibitors. Researches herein discover that both periplocoside G and periplocoside I have better intracellular IDO inhibitory activity than a positive control 1-MT (1-methyl-tryptophan), have significant IDO inhibitoryactivity, and are suitable for treating cancers, Alzheimer's disease, autoimmune diseases, ankylosing spondylitis, bacterial infections, cataract, mood disorders, and depression or anxiety.

Description

technical field [0001] The invention belongs to the field of medicines or health-care products, in particular to the use of C21 steroids in the preparation of IDO inhibitors. Background technique [0002] IDO (indoleamine-2,3-dioxygenase) is the only rate-limiting enzyme outside the liver that catalyzes the metabolism of tryptophan along the kynurenine pathway (KP). , tryptophan can be decomposed into various metabolites such as L-kynurenine, picolinic acid and quinolinic acid. L-tryptophan is an essential amino acid for maintaining cell activation and proliferation in the human body, and it is also an indispensable component of protein. L-tryptophan can lead to abnormal functions of some important cells. Since its discovery in 1967, the mechanism by which IDO inhibits the proliferation of pathogenic microorganisms by degrading tryptophan, and the relationship between IDO and neurological diseases have gradually been elucidated; and studies have confirmed that IDO is also i...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61P35/00A61P25/28A61P37/06A61P29/00A61P19/08A61P31/04A61P27/12A61P25/00A61P25/18A61P25/22A61P25/24
CPCA61K31/7048
Inventor 温尧林
Owner NANJING BAOHE BIOTECH
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